Cat. No.: HY-18006

NKP608

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NKP608 is a non-peptidic derivative of 4-aminopiperidine, a highly selective, orally active, neurokinin-1 (NK₁) receptor antagonist with IC₅₀ of 2.6 nM. NKP608 is active both in vitro and in vivo, showing extremely low affinity for NK₂, NK₃ receptors. NKP608 exerts its effects by blocking the NK₁ receptor, regulate cell proliferation and apoptosis, affect neurotransmitter functions and gastric mucosal repair mechanisms, and suppress the Wnt/β-catenin pathway in antitumor research. NKP608 is applicable to research related to various diseases, including cough, anxiety disorders, depression, gastric mucosal injury, and colorectal cancer.

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Pureté: 99.88%
CAS No.: 177707-12-9
Formule: C₃₁H₂₄ClF₆N₃O₂
Masse moléculaire:619.98

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

NKP608 Chemical Structure

CAS No.: 177707-12-9

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[7]

NK1R

2.6 nM (IC₅₀)

Wnt3A

Bcl-2

Caspase 3

Bax

Voir tous les produits spécifiques à Isoform Neurokinin Receptor :

Voir tous les produits spécifiques à Isoform Wnt :

Voir tous les produits spécifiques à Isoform Bcl-2 Family :

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In Vitro

NKP608 binds to human recombinant NK₁ receptor with a pK_i of 8.96, and shows lower affinity for human recombinant NK₂ (pK_i: 6.1) and NK₃ (pK_i: 6.25) receptors^[1].
NKP608 binds to NK₁ receptor in bovine retina (IC₅₀: 2.6 nM), gerbil midbrain (IC₅₀: 13 nM) and rat striatum (IC₅₀: 27 nM), and exhibits low affinity for NK₂ receptor in bovine bladder (IC₅₀: 2100 nM) and NK₃ receptor in gerbil cortex (IC₅₀: 1500 nM)^[5].
NKP608 (1 μM; 1 h) causes a 20-fold shift in the EC₅₀ of substance P-induced inositol phosphate synthesis in rat cloned NK₁ receptor-expressing CHO cells, and inhibits substance increase in acidification rate in rat NK₁ receptor-expressing CHO cells^[3].
NKP608 (0.001-100 μM; 72 h) inhibits proliferation of human colorectal cancer HCT116 cells in a concentration-dependent manner^[7].
NKP608 (10 μM; 24 h) inhibits migration and invasion of human colorectal cancer HCT116 cells.NKP608 induces apoptosis of human colorectal cancer HCT116 cells, downregulates the expression of Bcl-2, and upregulates the expression of Bax and Active-Caspase-3. NKP608 reduces the expression of Wnt-3a, β-catenin, Cyclin D1 and VEGF, and induces the expression of E-Cadherin in human colorectal cancer HCT116 cells^[7].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[7]

Cell Line:

HCT116 cells (human colorectal cancer)
Concentration:

0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 10 μM, 100 μM
Incubation Time:

72 h
Result:

Inhibits proliferation of HCT116 cells in a concentration-dependent manner.

Cell Proliferation Assay^[7]

Cell Line:

HCT116 cells (human colorectal cancer)
Concentration:

10 μM
Incubation Time:

24 h, 48 h, 72 h
Result:

Significantly inhibits migration of HCT116 cells.

Cell Invasion Assay^[7]

Cell Line:

HCT116 cells (human colorectal cancer)
Concentration:

10 μM
Incubation Time:

24 h
Result:

Significantly inhibits invasion of HCT116 cells.

Apoptosis Analysis^[7]

Cell Line:

HCT116 cells (human colorectal cancer)
Concentration:

10 μM
Incubation Time:

24 h
Result:

Induces apoptosis of HCT116 cells.

Western Blot Analysis^[7]

Cell Line:

HCT116 cells (human colorectal cancer)
Concentration:

10 μM
Incubation Time:

24 h
Result:

Downregulates expressions of Bcl-2, Wnt-3a, β-catenin, Cyclin D1 and VEGF; upregulates expressions of Bax, Active-Caspase-3 and E-Cadherin.

In Vivo

NKP608 (0.03, 0.3, 1 mg/kg; p.o.; once; 2 h prior to challenge) significantly reduces citric acid-induced cough in Dunkin Hartley guinea pigs^[1].
NKP608 (0.003, 0.03, 0.3 mg/kg; p.o.; once; 90 min prior to test) exerts anxiolytic-like effects in male spontaneously hypertensive rats (SHR) in the open field test and partial anxiolytic-like effects in male Lewis rats in the elevated plus-maze (EPM) test^[2].
NKP608 (0.2 mg/kg; i.v.; once; immediately prior to agonist challenge) potently inhibits GR73632 (HY-P1192)-induced foot drumming in Mongolian gerbils^[3].
NKP608 (0.01, 0.1, 0.3 mg/kg; p.o.; once; 2 h prior to test) increases social investigation time in Mongolian gerbils, showing robust anxiolytic effects^[4].
NKP608 (0.03-3 mg/kg; p.o.; once; 2, 5 or 24 h prior to agonist administration) dose-dependently inhibits SPOMe-induced hind foot thumping in Mongolian gerbils with ID₅₀ values of 0.23 mg/kg (2 h), 0.15 mg/kg (5 h) and 0.38 mg/kg (24 h), respectively^[5].
NKP608 (0.01-1 mg/kg; p.o.; once; 90 min prior to test) specifically increases active social interaction time in Sprague-Dawley rats in a highly illuminated unfamiliar arena^[5].
NKP608 (0.03-3 mg/kg; p.o.; once; 90 min prior to test) increases social exploration time of intruder rats towards resident rats in Sprague-Dawley rats^[5].
NKP608 (1 mg/kg; i.g.; once daily; for 8 consecutive days) delays gastric cryoulcer healing and decreases the number of Ki-67-positive epithelial cells in the ulcer margin in both wild-type and COX-2^-/- mice^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Dunkin Hartley guinea pigs (250-500 g; no gender specified) were exposed to nebulized citric acid (0.6 M) for 10 min to induce cough and airway obstruction^[1].
Dosage:

NKP608: 0.03, 0.3, 1 mg/kg; single drug administration
Administration:

Oral (p.o.) administration; once; 2 h prior to citric acid challenge
Result:

Significantly reduces the number of citric acid-induced coughs by 77% (0.03 mg/kg), 74% (0.3 mg/kg) and 79% (1 mg/kg), respectively; does not significantly reduce citric acid-induced increase in enhanced pause (Penh).

Animal Model:

Male spontaneously hypertensive rats (SHR) and male Lewis rats (9 weeks old; body weight: SHR males 232 g, LEW males 234 g) were subjected to elevated plus-maze (EPM) and open field (OF) tests to evaluate anxiety-related behaviors^[2].
Dosage:

0.003, 0.03, 0.3 mg/kg
Administration:

Oral (p.o.) administration; once; 90 min prior to tests
Result:

Exerts anxiolytic-like effects in male SHR rats in the OF test.
Shows partial anxiolytic-like effects in male Lewis rats in the EPM test .
Has no significant anxiolytic effects in female SHR or Lewis rats in either test.

Animal Model:

Mongolian gerbils (40-60 g; no gender specified) were intracerebroventricularly (i.c.v.) injected with GR73632 (3 pmol/5 μL) to induce foot drumming behavior^[3].
Dosage:

0.2 mg/kg
Administration:

Intravenous (i.v.) injection; once; immediately prior to GR73632 administration
Result:

Potently inhibits GR73632-induced foot drumming in Mongolian gerbils.

Animal Model:

Mongolian gerbils (70-85 g; male) were subjected to the social investigation test to evaluate anxiety-related behaviors^[4].
Dosage:

0.01, 0.1, 0.3 mg/kg
Administration:

Oral (p.o.) administration; once; 2 h prior to test
Result:

Increases the time of social investigation towards an untreated, unfamiliar partner.

Animal Model:

Mongolian gerbils (70-80 g; male) were intracerebroventricularly (i.c.v.) injected with SPOMe (1 μg/5 μL) to induce hind foot thumping behavior^[5].
Dosage:

0.1, 0.3 mg/kg
Administration:

Oral (p.o.) administration; once daily; for 7 consecutive days
Result:

Attenuates SPOMe-induced hind foot thumping when tested 2 h or 24 h after the last administration.

Animal Model:

Sprague-Dawley rats (180-200 g; male) were subjected to the social interaction test in a highly illuminated unfamiliar arena (65×65×45 cm)^[5].
Dosage:

0.001 mg/kg, 0.01 mg/kg, 0.1 mg/kg, 1 mg/kg
Administration:

Oral (p.o.) administration; once; 90 min prior to test
Result:

Specifically increases active social interaction time between unfamiliar rats and does not affect general activity parameters.

Animal Model:

Wild-type and COX-2^-/- mice (20-24 g; female; 7-8 weeks old) were subjected to laparotomy to induce gastric cryoulcers via serosal application of a CO₂-cooled cryoprobe (15 s)^[6].
Dosage:

1 mg/kg
Administration:

Intragastric (i.g.) administration; once daily; for 8 consecutive days
Result:

Delays gastric cryoulcer healing in both wild-type and COX-2⁻/⁻ mice and decreases the number of Ki-67-positive epithel.

Animal Model:

Sprague-Dawley rats (residents: 350-400 g, male; intruders: 100-120 g, male, Lister Hooded strain) were subjected to the social exploration test^[5].
Dosage:

0.03 mg/kg, 0.3 mg/kg, 3 mg/kg
Administration:

Oral (p.o.) administration; once; 90 min prior to test (administered to intruder rats only)
Result:

Increases the time of active social exploration of intruder rats towards resident rats.

Chemical Information

CAS No. 177707-12-9
Appearance Solid
Masse moléculaire 619.98
Formule C₃₁H₂₄ClF₆N₃O₂
Color Light yellow to yellow
SMILES

O=C(C1=CC=NC2=CC=CC=C12)N[C@@H]3C[C@@H](CC4=CC=C(Cl)C=C4)N(C(C5=CC(C(F)(F)F)=CC(C(F)(F)F)=C5)=O)CC3
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Biol Res

The NK1 receptor antagonist NKP608 inhibits proliferation of human colorectal cancer cells via Wnt signaling pathway. [Abstract]

2018 May 30;51(1):14. PMID: 29843798

NKP608 purchased from MedChemExpress. Usage Cited in: Biol Res. 2018 May 30;51(1):14. [Abstract]

Effect of NKP608 on the expression of Bax, Bcl-2 and Caspase-3 protein are detected by western blot assay

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (161.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6130 mL

8.0648 mL

16.1296 mL

5 mM

0.3226 mL

1.6130 mL

3.2259 mL

10 mM

0.1613 mL

0.8065 mL

1.6130 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

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Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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Références

[1]. El-Hashim AZ, Wyss D, Lewis C. Effect of a novel NK1 receptor selective antagonist (NKP608) on citric acid induced cough and airway obstruction. Pulm Pharmacol Ther. 2004;17(1):11-8. [Content Brief]

[2]. Vendruscolo LF, Takahashi RN, Brüske GR, Ramos A. Evaluation of the anxiolytic-like effect of NKP608, a NK1-receptor antagonist, in two rat strains that differ in anxiety-related behaviors. Psychopharmacology (Berl). 2003 Nov;170(3):287-93. [Content Brief]

[3]. Rupniak NM, Carlson EJ, Shepheard S, et al. Comparison of the functional blockade of rat substance P (NK1) receptors by GR205171, RP67580, SR140333 and NKP-608. Neuropharmacology. 2003 Aug;45(2):231-41. [Content Brief]

[4]. Gentsch C, Cutler M, Vassout A, et al. Anxiolytic effect of NKP608, a NK1-receptor antagonist, in the social investigation test in gerbils. Behav Brain Res. 2002 Jul 18;133(2):363-8. [Content Brief]

[5]. Vassout A, Veenstra S, Hauser K, et al. NKP608: a selective NK-1 receptor antagonist with anxiolytic-like effects in the social interaction and social exploration test in rats. Regul Pept. 2000 Dec 22;96(1-2):7-16. [Content Brief]

[6]. Schmassmann A, et al. Expression of functional neurokinin-1 receptors in regenerative glands during gastric wound healing in rodents. Gastroenterology. 2004 Mar;126(3):784-95. [Content Brief]

[7]. Niu XL, et al. The NK1 receptor antagonist NKP608 inhibits proliferation of human colorectal cancer cells via Wnt signaling pathway. Biol Res. 2018 May 30;51(1):14. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.6130 mL	8.0648 mL	16.1296 mL	40.3239 mL
	5 mM	0.3226 mL	1.6130 mL	3.2259 mL	8.0648 mL
	10 mM	0.1613 mL	0.8065 mL	1.6130 mL	4.0324 mL
	15 mM	0.1075 mL	0.5377 mL	1.0753 mL	2.6883 mL
	20 mM	0.0806 mL	0.4032 mL	0.8065 mL	2.0162 mL
	25 mM	0.0645 mL	0.3226 mL	0.6452 mL	1.6130 mL
	30 mM	0.0538 mL	0.2688 mL	0.5377 mL	1.3441 mL
	40 mM	0.0403 mL	0.2016 mL	0.4032 mL	1.0081 mL
	50 mM	0.0323 mL	0.1613 mL	0.3226 mL	0.8065 mL
	60 mM	0.0269 mL	0.1344 mL	0.2688 mL	0.6721 mL
	80 mM	0.0202 mL	0.1008 mL	0.2016 mL	0.5040 mL
	100 mM	0.0161 mL	0.0806 mL	0.1613 mL	0.4032 mL

NKP608

1 Cited Publications

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NKP608

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Neuronal Signaling Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Pyroptosis Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Neuroprotective Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Mitochondria-Targeted Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cytokine Inhibitors Library

Cell Death Library

Extracellular Vesicles (EVs) Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) NKP608

Voir tous les produits spécifiques à Isoform Neurokinin Receptor

Voir tous les produits spécifiques à Isoform Wnt

Voir tous les produits spécifiques à Isoform Bcl-2 Family

Voir tous les produits spécifiques à Isoform VEGFR

Voir tous les produits spécifiques à Isoform Caspase

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

NKP608 Related Classifications

HY-18006 Related Classifications